Novel Mannich Bases of Benzimidazole Derivatives: An Antibacterial Study of Environmental Bacterial Strains

A previous study was conducted on the synthesis and antibacterial evaluation of Mannich bases of 2-(thioalkyl)-1H-methylbenzimidazole derivatives. The results of this study showed that certain 2-(thioalkyl)-1H-methylbenzimidazole and 2-(thioalkyl)-methyl-1-(piperidin-1-ylmethyl)benzimidazole derivatives possess antibacterial activities against clinical strains, such as Escherichia coli, Klebsiella pneumonia (Gram-negative bacteria), Staphylococcus aureus and Pseudomonas aeruginosa (Gram-positive bacteria). Following these favorable results, we extended the antibacterial evaluation of this series of molecules to environmental strains. The aim of this study was to assess the impact of the methyl-piperidine group fixed at position-1 of this new series of benzimidazoles on the antibacterial activity of environmental strains. In addition, we first evaluated the antibacterial activity of four 2-(thioalkyl)methylbenzimidazole derivatives and then that of five 2-(thioalkyl)-methyl-1-(piperidin-1-ylmethyl) benzimidazole derivatives. This study allowed us to show that compounds 1d and 1e could inhibit bacterial growth in vitro of the Enterobacteria P1 strain with inhibition diameters of 17.3 ± 0.6 mm and 10 ± 0.0 mm, respectively. However, addition of methyl-piperidinyl in this series showed that five (5) of 2-(thioalkyl)-methyl-1-(piperidin-1-ylmethyl) benzimidazole derivatives had an inhibitory effect on the in vitro growth of bacterial strains used except on Enterobacteria P2 with inhibition diameters between 10.0 ± 0.8 mm and 27.9 ± 1.4 mm. The introduction of the methyl-piperidinyl group at the 1-position of 2-(thioalkyl)-1H-methylbenzimidazole derivatives greatly improved the antibacterial activity against environmental bacteria such as Escherichia coli A1, A2, A3, and A4 and two Enterobacteria P1.

Synthesis and Biological Activities of Some Mannich Bases of 5-(4-Hydroxyphenyl)-1,3,4-Oxadiazole-2-Thione

以对羟基苯甲酸乙酯为原料，经肼解、环化合成５（４羟基苯基）１，３，４二唑２硫酮，继而经Ｍａｎｎｉｃｈ反应合成了四种新曼尼希碱，其结构经红外光谱、核磁共振和元素分析证实。初步抑菌活性试验表明，显示弱的抑菌活性。

Synthesis and NO production inhibition of novel Mannich base derivatives of irisolidone

Five new C-8 Mannich base derivatives of irisolidone 2a-2e were synthesized and their nitric oxide（NO）production inhibitory activity was evaluated.Compounds 2a,2b,2c and 2e displayed stronger activities in vitro than the parent compound irisolidone.

Geographic Drone-based Route Optimization Approach for Emergency Area Ad-Hoc Network

Wireless sensor Mobile ad hoc networks have excellent potential in moving and monitoring disaster area networks on real-time basis.The recent challenges faced in Mobile Ad Hoc Networks(MANETs)include scalability,localization,heterogeneous network,self-organization,and self-sufficient operation.In this background,the current study focuses on specially-designed communication link establishment for high connection stability of wireless mobile sensor networks,especially in disaster area network.Existing protocols focus on location-dependent communications and use networks based on typically-used Internet Protocol(IP)architecture.However,IP-based communications have a few limitations such as inefficient bandwidth utilization,high processing,less transfer speeds,and excessive memory intake.To overcome these challenges,the number of neighbors(Node Density)is minimized and high Mobility Nodes(Node Speed)are avoided.The proposed Geographic Drone Based Route Optimization(GDRO)method reduces the entire overhead to a considerable level in an efficient manner and significantly improves the overall performance by identifying the disaster region.This drone communicates with anchor node periodically and shares the information to it so as to introduce a drone-based disaster network in an area.Geographic routing is a promising approach to enhance the routing efficiency in MANET.This algorithm helps in reaching the anchor(target)node with the help of Geographical Graph-Based Mapping(GGM).Global Positioning System(GPS)is enabled on mobile network of the anchor node which regularly broadcasts its location information that helps in finding the location.In first step,the node searches for local and remote anticipated Expected Transmission Count(ETX),thereby calculating the estimated distance.Received Signal Strength Indicator(RSSI)results are stored in the local memory of the node.Then,the node calculates the least remote anticipated ETX,Link Loss Rate,and information to the new location.Freeway Heuristic algorithm improves the data speed,efficiency and determines the path and optimization problem.In comparison with other models,the proposed method yielded an efficient communication,increased the throughput,and reduced the end-to-end delay,energy consumption and packet loss performance in disaster area networks.

BIODRILL S合成基钻井液在垦利区块首次应用

渤海油田垦利9-1区块地层岩性复杂,且存在断层带,钻井过程中易发生泥岩水化分散和砂岩层井眼缩径等问题,井壁垮塌风险极大。针对该区块地层岩性特点和技术难题并结合环保要求,制备了一种复合型封堵材料PFMOSHIELD,构建了BIODRILL S合成基钻井液体系。该体系流变性能良好,抗钙、抗岩屑污染达26%和15%,封堵性、沉降稳定性、润滑性优异,高温高压砂盘滤失量3.2 mL,静置7 d沉降因子为0.53,极压润滑系数0.082。BIODRILL S首次在渤海湾垦利9-1区块进行了现场应用,结果表明:该体系解决了垦利9-1区块泥页岩水化和砂岩层井眼缩径问题,垦利9-1北-3定向探井三开井段上部地层钻屑完整,钻屑达4~7 cm;井眼清洁性能良好,钻井液动塑比超过0.59 Pa/mPa·s,φ6和φ3读数均超过9,剪切稀释性强,提高了井眼净化效率,有效避免形成“岩屑床”;润滑性能优异,在大井斜段(55°、70°、67°)可实现直接起钻。

COMBINATORIAL SYNTHESIS OF MANNICH BASES IN SOLUTION/POLYMER REAGENT WORKUP

This paper describes a combinatorial Synthesis of the Mannich Bases in Solution through the Mannich reaction using 3 ketones, 5 amines and formaldehyde in solution and hydrochloride as a catalyst and then using a macroporous quarterized ammonium resin (CO32- form) as a scavenge agent to remove the acid catalyst when the Mannich reaction is completed. It was found by GC/MS analysis that the symmetrical ketone, such as acetone, in the Mannich reaction mainly produces one Mannich base; while the asymmetrical ketone, such as 2-pentanone, gives two Mannich bases. The reactivity depends on the tereo-hinder of both ketones and amines.

COVID-19 mortality paradox(United States vs Africa):Mass vaccination vs early treatment

The coronavirus disease 2019(COVID-19)mortality rate in 55 African countries is almost 4.5 times lower than in the coronavirus disease 2019(COVID-19)despite Africa having over 4.2 times more people.This mortality paradox is also evident when comparing Nigeria,a heavily populated,poorly vaccinated and weakly mandated country to Israel,a small,highly vaccinated and strictly mandated country.Nigeria has almost 4 times lower COVID mortality than Israel.In this Field of Vision perspective,I explain how this paradox has evolved drawing upon my academic,clinical and social experience.Since April 2020,I’ve developed and been using the Egyptian immune-modulatory Kelleni’s protocol to manage COVID-19 patients including pediatric,geriatric,pregnant,immune-compromised and other individuals suffering from multiple comorbidities.It’s unfortunate that severe acute respiratory syndrome coronavirus 2 is still evolving accompanied by more deaths.However in Africa,we’ve been able to live without anxiety or mandates throughout the pandemic because we trust science and adopted early treatment using safe,and effective repurposed drugs that have saved the majority of COVID-19 patients.This article represents an African and Egyptian tale of honor.

Mannich-Type Reactions of Aldimines and Hetero Diels-Alder Reactions of Aldehydes Catalyzed by Anion-Type Lewis Bases Derived from a Single Molecule

Mannich-type reactions of aldimines with silyl enolates and hetero Diels-Alder reactions of aldehydes with Danishef-sky’s diene in the presence of anion catalysts derived from proline were performed to afford the corresponding products in high yields.

新型多取代Trger’s base衍生物的合成及其晶体结构

以邻氨基二苯甲酮为原料,经两分子环化缩合反应制得6,12-二芳基二苯并[b,f][1,5]二氮杂环辛四烯(2a^2d);2a^2d经Li Al H4还原制得6,12-二芳基-5,6,11,12-四氢二苯并[b,f][1,5]二氮杂环辛(3a^3d);3a^3d与醛(或酮)反应,合成了一系列新型的多取代Trger’s base衍生物(4a^4d和5a^7a),其结构经1H NMR,13C NMR,HR-MS(ESI)和X-射线单晶衍射表征。通过分析架桥前后3a(CCDC:1498564)和6a(CCDC:1498555)的晶体结构,解释了该类化合物1H NMR中NCH质子及桥上取代基质子裂分的原因,并进一步证实了4~7为非C2轴对称结构。

新型含均三氮唑Schiff碱吡唑基Mannich碱的合成

以N-(1-苯基-3-甲基-5-氯)吡唑甲酰肼基二硫代甲酸钾和水合肼为起始原料,经闭环反应制得4-氨基-5-(1-苯基-3-甲基-5-氯吡唑)-1,2,4-三唑-3-硫酮(2);2与对溴苯甲醛经缩合反应得4-(4-溴苯次甲亚胺)-5-(1-苯基-3-甲基-5-氯吡唑)-1,2,4-三唑-3-硫酮(3);以乙醇为溶剂,3在甲醛溶液中与吗啉于75℃反应4 h合成了新化合物——2-(吗啉亚甲基)-4-(4-溴苯次甲亚胺)-5-(1-苯基-3-甲基-5-氯吡唑)-1,2,4-三唑-3-硫酮,总收率37%,其结构经1H NMR,IR和元素分析表征。

新型含2,4-二氯苯基-1,2,4-三唑Schiff碱Mannich碱衍生物的合成及生物活性

3-巯基-4-氨基-5-(2,4-二氯)苯基-1,2,4-三唑与取代苯甲醛经缩合反应制得中间体4-(取代苯次甲亚胺基)-5-(2,4-二氯苯基)-4H-1,2,4-三唑-3-硫酮(3a^3d);3a^3d在甲醛溶液中分别与吗啉于75℃反应4 h合成了4个新型的含2,4-二氯苯基均三氮唑Schiff碱Mannich碱衍生物——4-(取代苯甲亚胺基)-5-(2,4-二氯苯基)-2-(吗啉亚甲基)-2H-1,2,4-三唑-3-硫酮,收率69%~81%,其结构经1H NMR,13C NMR,IR及元素分析表征。初步生物活性测试结果表明:部分目标化合物在用药量为100 mg·L-1时对黄瓜霜霉病的抑制率达100%。

基于Faster R-CNN的密集人群检测算法

为提高拥挤场景下的人群检测准确率,提出一种基于改进Faster R-CNN的密集人群检测算法。首先,在特征提取阶段添加空间与通道注意力机制,使用加强的双向特征金字塔网络(S-BiFPN)替代原网络中的多尺度特征金字塔(FPN),使网络对重要特征进行自主学习并加强对图像深层特征的提取;其次,引入多实例预测(MIP)算法对实例进行预测,以避免模型对拥挤场景下的目标造成漏检;最后,对模型中的非极大值抑制(NMS)进行优化,并额外增设一个交并比(IoU)阈值,以对检测结果的干扰项进行精确抑制。在开源的密集人群检测数据集上进行测试的结果显示,相较于原Faster R-CNN算法,所提算法的平均精度(AP)提升5.6%,Jaccard指数值提升3.2%。所提算法具有较高检测精度和稳定性,可以满足密集场景人群检测的需求。

A New Investigation of Mannich Reaction

During the synthesis of the derivatives of styryl ketonic Mannich bases, a side -product IM,other than the normal Mannich base MA, is obtained. Mannich reaction is further studied and the formation mechanism of product IM is postulated and discussed on the basis of deuterium labelling.

Li_(2)S掺杂对富锂锰基材料首次库仑效率的提升效果研究

富锂锰基材料(LRM)由于电压平台高、比容量高,在锂电池材料研究中受到广泛关注。针对富锂锰基材料首次充放电库仑效率较低的问题,采用Li_(2)S对富锂锰基材料(LRM)进行掺杂改性制备得到LRM-S材料。结果表明:LRM和LRM-S的晶体结构相近,具有层状晶体结构。扫描电镜分析表明,LRM-S材料由10~20nm的一次颗粒团聚而成。元素分析表明LRM-S材料中含有均匀分散的S元素。电化学分析表明,LRM的首次充电比容量为291.80mAh/g,首次放电比容量为188.63mAh/g,首次库仑效率为64.64%。Li_(2)S掺杂改性材料LRM-S的首次充电比容量为387.04mAh/g,首次放电比容量为272.64mAh/g,首次库仑效率为70.44%,在首次充放电比容量和效率方面均有显著提升。

Electronic Structures and Spectra of the Bases and Base Pairs of Nucleic Acids

The present paper covers electronic structures and spectra of the bases and the base pairs of nucleic acids calculated by using the INDO/S method. For free bases we give the energy levels of ground states and transition energies of low-lying excited states and discuss the band characters. The results indicate that the calculated spectra are in good agreement with experimental values. On the other hand, our calculations for A-T and G-C pairs are very beneficial to understanding hydrogen bond properties of these pairs.

Some Novel Schiff Bases from Pyruvic Acid with Amines Containing N &S Donor Atoms: Synthesis, Spectral Studies and X-Ray Crystal Structures

Four Schiff bases, from pyruvic acid (1) with amines containing N and S donor atoms, thiocarbohydrazide (2, 61%), 2-methyl-3-thiosemicarbazide (3, 26%), S-benzyldithiocarbazate (4, 51%) and S-n-octyldithiocarbazate (5, 63%) have been successfully synthesized. The conventional method was used and a series of novel linear and cyclic Schiff bases were obtained with or without catalyst. All the Schiff bases were fully characterized by CHN elemental analysis, FT-IR, 1H & 13C NMR, EI-MS and two of the Schiff bases were further characterized by X-ray crystallographic structure analysis. Compound 2 crystallizes in the triclinic space group P-1 and unit cell dimensions are: a = 4.1777(8), b = 5.9538(11), c = 13.458(3) Å, α = 92.759(6), β = 90.813(6), γ = 100.040(6)°, R1 = 0.0439. Compound 3 crystallizes in the orthorhombic space group P n a 2(1) and unit cell dimensions are: a = 5.5992(2), b = 11.3962(5), c = 10.6473(5), α = 92.759(6), β = 90.813(6), γ = 100.040(6)°, R1 = 0.0285. Compounds 2 and 3 were obtained as cyclic Schiff bases which are triazine derivatives.

Mathematical Model of Natural Gas Desulfurization Based on Membrane Absorption

Models of mass transfer kinetics combined with mass transfer differential equation and mass transfer resistance equation were established on the basis of double-film theory. Mass transfer process of H2 S absorption by means of polypropylene hydrophobic microporous hollow fiber membrane contactor was simulated using MDEA(N-methyldiethanolamine) as the absorption liquid and corresponding experiments of natural gas desulfurization were performed. The simulation results indicated that the removal rate of hydrogen sulfide showed positive dependence on the absorption liquid concentration and gas pressure. However, the desulfurization rate showed negative dependence on gas flow. The simulated values were in good agreement with the experimental results. The in-tube concentration of hydrogen sulfide at the same point increased with increase in the gas velocity. Axial concentration of hydrogen sulfide decreased rapidly at the beginning, and the decrease saw a slowdown during the latter half period. Hydrogen sulfide concentration dropped quickly in the radial direction, and the reduction in the radial direction was weakened with the increase of axial length due to the gradual reduction of hydrogen sulfide concentration along the tube. The desulfurization rate under given operating conditions can be predicted by this model, and the theoretical basis for membrane module design can also be provided.

Synthesis and mesomorphic properties of fluorinated Schiff's base liquid crystals containing vinyl end groups

Three kinds of fluorinated Schiff＇s base esters, 4-allyloxy-2-X-6-X-benzoic acid 4-[（2, 3, 4-trifluorophenylimino）methyl]phenyl ester, where X=H or F, were synthesized and characterized. Their chemical structures were identified by Fourier transform infrared spectroscopy （FTIR） and ^1H nuclear magnetic resonance （^1H NMR）. Their mesomorphic properties were studied by polarized optical microscopy （POM） and differential scanning calorimetry （DSC）. It was found that all the three compounds exhibited enantiotropic nematic phases only. And their cleating point temperature and thermal range of mesophase decreased with the number of fluorine atoms on the rigid core of the compounds; while their melting point temperature showed no distinct regularity.

Individualized music for dementia:Evolution and application of evidence-based protocol

The theory-based intervention of individualized music has been evaluated clinically and empirically leading to advancement and refinement of an evidence-based protocol, currently in its 5th edition. An expanded version of the protocol was written for professional health care providers with a consumer version tailored for family caregivers. The underlying mid-range theory is presented along with a seminal study that was followed by further research in the United States, Canada, Great Britain, France, Sweden, Norway, Japan and Taiwan. Key studies are summarized. Given its efficacy when implemented by research staff, studies have advanced to testing the intervention under real-life conditions when implemented and evaluated by trained nursing assistants in long-term care facilities and visiting family members. In addition, one study evaluated the implementation of music by family members in the home setting. Initial research focused on agitation as the dependent variable with subsequent research indicating a more holistic response such as positive affect, expressed satisfaction, and meaningful interaction with others. The article advances by describing on-line programs designed to train health care professionals in the assessment, implementation and evaluation of individualized music. In addition, Gerdner has written a story for apicture book intended for children and their families(in press). The story models principles of individualized music to elicit positive memories, reduce anxiety and agitation, and promote communication. The article concludes with implications for future research.